This invention relates to certain dihydropyridines, specifically to certain 1,4-dihydropyridines having a basic substituted-amino containers group attached to the 2-position, which have utility as anti-ischaemic and antihypertensive agents.
The compounds of the invention delay or prevent the cardiac contracture which is believed to be caused by an accumulation of intracellular calcium under ischaemic conditions (Henry, P. D. et al., Am. J. Physiol. 233, H677, 1977). Calcium overload, during ischaemia, can have a number of additional adverse effects which would further compromise the ischaemic myocardium. These include less efficient use of oxygen for ATP production (Peng, C. F. et al., Circ. Res. 41, 208, 1977), activation of mitochondrial fatty acid oxidation (Otto, D. A. and Ontko, J. A., J. Biol. Chem., 253, 789, 1978), and possibly, promotion of cell necrosis (Wrogemann, K. and Pena, S. D. J. Lancet Mar. 27, p. 672, 1976). Thus the compounds are useful in the treatment or prevention of cardiac conditions, such as angina pectoris, cardiac arrythmias, heart attacks and cardiac hypertrophy. The compounds also possess vasodilator activity and are thus useful as antihypertensives and for the treatment of coronary vasospasm.